Abstract <p>Preparative methods were developed for the synthesis of 4,7-diaryl-3,4-dihydropyrido[4,3-<i>d</i>]pyrimidin-2(1<i>H</i>)-ones based on readily available Biginelli products. Optimal conditions for the reaction of 4-aryl-6-styryltetrahydropyrimidine-5-carbaldehydes with ammonium salts were selected, enabling the preparation of substituted pyrido[4,3-<i>d</i>]pyrimidinones in yields up to 57%. An alternative synthetic route involving oxime formation followed by cyclization under the action of DBU was also studied.</p>

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Synthesis of 4,7-Diaryl-3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-ones

  • Anastasia M. Uryadova,
  • Elena S. Makarova,
  • Sergey I. Filimonov,
  • Zhanna V. Chirkova

摘要

Abstract

Preparative methods were developed for the synthesis of 4,7-diaryl-3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-ones based on readily available Biginelli products. Optimal conditions for the reaction of 4-aryl-6-styryltetrahydropyrimidine-5-carbaldehydes with ammonium salts were selected, enabling the preparation of substituted pyrido[4,3-d]pyrimidinones in yields up to 57%. An alternative synthetic route involving oxime formation followed by cyclization under the action of DBU was also studied.